Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
DOLUTEGRAVIR, EMTRICITABINE and TENOFOVIR ALAFENAMIDE vs EMTRIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) that blocks viral DNA integration. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that terminates viral DNA chain elongation. Tenofovir alafenamide is an NRTI that inhibits HIV reverse transcriptase after intracellular conversion to tenofovir diphosphate.
Nucleoside reverse transcriptase inhibitor; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (50 mg dolutegravir/200 mg emtricitabine/25 mg tenofovir alafenamide) taken orally once daily with or without food.
Emtricitabine 200 mg orally once daily.
None Documented
None Documented
Dolutegravir: ~14 hours (single dose), ~12 hours (steady state). Emtricitabine: ~10 hours. Tenofovir alafenamide: ~0.5 hours (parent), but its active metabolite tenofovir diphosphate has intracellular half-life >60 hours. Clinically, tenofovir alafenamide is dosed once daily due to intracellular accumulation.
Terminal elimination half-life ~10 hours (mean 10 h, range 7-14 h) in adults; prolonged in renal impairment (up to 90 h in severe impairment)
Dolutegravir: ~64% feces (as parent), ~31% urine (as glucuronide conjugate, <1% parent). Emtricitabine: ~86% urine (as parent and metabolites), ~14% feces. Tenofovir alafenamide: <1% renal (as parent), ~82% feces (as metabolite tenofovir).
Renal excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI